Comparative Pharmacology
Head-to-head clinical analysis: LISDEXAMFETAMINE DIMESYLATE versus METHYLIN.
Head-to-head clinical analysis: LISDEXAMFETAMINE DIMESYLATE versus METHYLIN.
LISDEXAMFETAMINE DIMESYLATE vs METHYLIN
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Lisdexamfetamine is a prodrug of dextroamphetamine, which blocks the reuptake of norepinephrine and dopamine from the synaptic cleft and increases their release into the extraneuronal space.
Methylphenidate is a central nervous system stimulant. It blocks the reuptake of dopamine and norepinephrine into presynaptic neurons, increasing their concentrations in the synaptic cleft.
30–70 mg orally once daily in the morning.
10 mg orally twice daily, administered 4-6 hours apart; doses may be adjusted in 5-10 mg increments weekly up to 60 mg/day.
None Documented
None Documented
Terminal elimination half-life of lisdexamfetamine is approximately 1 hour (prodrug conversion), while dextroamphetamine (active moiety) has a half-life of 10-12 hours in adults. In children, half-life is slightly shorter (9-11 hours). Clinically, once-daily dosing provides symptom control for ADHD.
2-4 hours (short elimination half-life, requiring multiple daily dosing; immediate-release: 3-4 hours, extended-release: 3-6 hours)
Primarily renal: approximately 95% of the dose is excreted in urine, with about 70% as intact lisdexamfetamine, 20% as dextroamphetamine and its metabolites (hippuric acid, benzoic acid), and minimal biliary/fecal elimination (<5%).
Renal: 90% (mainly as metabolites, 30-50% as unchanged drug); fecal: <1%
Category C
Category C
CNS Stimulant
CNS Stimulant